产品说明书

Lumiracoxib

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Chemical Structure| 220991-20-8 同义名 : COX-189
CAS号 : 220991-20-8
货号 : A112255
分子式 : C15H13ClFNO2
纯度 : 98%
分子量 : 293.721
MDL号 : MFCD07186254
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(408.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • COX-2

    COX-2, Ki:60 nM

  • COX-1

    COX-1, Ki:3 μM
描述 Lumiracoxib is a selective cyclooxygenase (COX)-2 inhibitor that possesses a carboxylic acid group that makes it weakly acidic. It has good oral bioavailability; maximum plasma concentrations are reached two hours after oral administration. Lumiracoxib has been found to be effective at doses of 100 - 400 mg once a day for chronic pain and 400 mg/day for acute pain. In comparison to NSAIDs (nonsteroidal anti-inflammatory drugs), patients taking lumiracoxib experience significantly fewer adverse events and greater tolerability[3]. In single- and multiple-dose well designed trials in patients with acute pain associated with primary dysmenorrhoea, dental or orthopaedic surgery or tension-type headache, lumiracoxib 100 - 800 mg once daily was more effective in relieving acute pain than placebo or controlled-release oxycodone 20 mg, and was at least as effective as selective COX-2 inhibitors or nonselective NSAIDs[4]. COX-2 selectivity of lumiracoxib is associated with a reduced incidence of gastroduodenal erosions compared with naproxen and a lack of effect on both small and large bowel permeability[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.40mL

0.68mL

0.34mL

17.02mL

3.40mL

1.70mL

34.05mL

6.81mL

3.40mL
参考文献

[1]Dickie AP, Wilson CE, et al. The pharmacokinetics and metabolism of lumiracoxib in chimeric humanized and murinized FRG mice. Biochem Pharmacol. 2017 Jul 1;135:139-150.

[2]Esser R, Berry C, et al. Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50.

[3]Buvanendran A, Barkin R. Lumiracoxib. Drugs Today (Barc). 2007;43(3):137-147

[4]Lyseng-Williamson KA, Curran MP. Lumiracoxib. Drugs. 2004;64(19):2237-2248

[5]Rordorf CM, Choi L, Marshall P, Mangold JB. Clinical pharmacology of lumiracoxib: a selective cyclo-oxygenase-2 inhibitor. Clin Pharmacokinet. 2005;44(12):1247-1266